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Pharmacological Activity from US Patent US11136337: "Pyrazole- and indazole-substituted oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors"
Assay data:42 Active, 23 Activity ≤ 1 nM, 42 Activity ≤ 1 µM, 42 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition Assay from US Patent US8957075: "O-GlcNAc transferase inhibitors and uses thereof"
Assay data:15 Active, 1 Activity ≤ 1 µM, 26 Tested
Inhibition of catalytic activity of OGT (unknown origin) using EA2 peptide as substrate incubated for 30 mins by HPLC-based enzyme assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of OGT (unknown origin) at 1 mM using UDP-GlcNAc as substrate measured after 2 hrs by UDP-Glo luminescence assay relative to control
Assay data:22 Tested
Inhibition of OGT (unknown origin) using UDP-GlcNAc as substrate measured after 2 hrs by UDP-Glo luminescence assay
Assay data:9 Tested
Competitive inhibition of OGT (unknown origin) at 0.5 mM in presence of RBL_2_410_422 peptide by microarray analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Noncompetitive inhibition of OGT (unknown origin) using fixed UDP-GlcNAc levels and variable CKII peptide level by UDP-Glo glycosyltransferase assay
Assay data:2 Tested
Noncompetitive inhibition of OGT (unknown origin) using variable UDP-GlcNAc levels and fixed CKII peptide level by UDP-Glo glycosyltransferase assay
Inhibition of OGT (unknown origin) assessed as reduction in GlcNAc transfer to CKII peptide at 1000 uM incubated for 60 mins by HPLC method
Inhibition of OGT (unknown origin) assessed as reduction in GlcNAc transfer to CKII peptide at 4000 uM incubated for 60 mins by HPLC method
Inhibition of OGT (unknown origin) assessed as reduction in GlcNAc transfer to CKII peptide incubated for 60 mins by HPLC method
Assay data:13 Tested
Inhibition of OGT (unknown origin) assessed as reduction in GlcNAc transfer to CKII peptide at 1 mM incubated for 60 mins by HPLC method based inactivation time course analysis
Assay data:3 Tested
Binding affinity to OGT (unknown origin) assessed as modification at Cys531/Cys620 residues following in-gel trypsin digestion by LC/MS/MS method
Assay data:11 Active, 13 Tested
Binding affinity to OGT (unknown origin) assessed as modification at Cys590 residues following in-gel trypsin digestion by LC/MS/MS method
Inhibition of OGT (unknown origin) assessed as reduction in GlcNAc transfer to CKII peptide at 100 uM incubated for 60 mins by HPLC method
Binding affinity to OGT (unknown origin) assessed as tethering of Cys921 and Cys927 residues at 4 mM at 37 degC for 2 hrs in presence of Tris-HCL buffer containing 1 mM DTT by SDS-PAGE method
Binding affinity to OGT (unknown origin) assessed as tethering of cysteine residues at 4 mM at 37 degC for 2 hrs in presence of Tris-HCL buffer containing 1 mM DTT by SDS-PAGE method
Inhibition of OGT (unknown origin)
SummaryRelated BioAssays by Target
Inhibition of nucleocytoplasmic OGT (unknown origin)
Assay data:1 Active, 3 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Inhibition of OGT in human HeLa cells assessed as decrease in intracellular O-GlcNAcylated protein level up to 500 uM after 24 to 48 hrs by immunoblot analysis
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